The satiating effect of the selective cholecystokininA (CCKA) receptor agonist A71378 and the mixed A and B receptor agonist CCK-8S were compared in 24-h food-deprived rats. After systemic application of 1.6, 8.0, and 40 micrograms/kg A71378 or CCK-8S, respectively, food intake was measured for 24 h. During the first hour A71378 and CCK-8S decreased food intake similarly. Two and 4 h after treatment, the satiating effect of A71378 continued. In contrast, 2 h after administration of CCK-8S a slight effect was observed at the highest dose (40 micrograms/kg), which totally disappeared after 4 h. In summary, the effect of A71378 on food intake is longer lasting compared to CCK-8S.
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http://dx.doi.org/10.1016/0196-9781(95)02131-0 | DOI Listing |
Diabetes Metab
January 2025
Division of Diabetes, Nutrition and Metabolic Disorders, CHU Liège, Liège, Belgium; Division of Clinical Pharmacology, Centre for Interdisciplinary Research on Medicines (CIRM), Liège University, Liège, Belgium. Electronic address:
Background: Obesity is an increasing public health problem because of its high prevalence and associated morbidity and mortality. Two weight-loss strategies are currently used, either bariatric surgery or pharmacological therapy with glucagon-like peptide-1 receptor agonists (GLP-1RAs). Preclinical studies in rodents suggested an increased risk of additive disorders after bariatric surgery contrasting with a reduced risk with GLP-1RAs.
View Article and Find Full Text PDFJ Steroid Biochem Mol Biol
January 2025
Department of Medicine, Washington University School of Medicine, St. Louis, MO, USA; Department of Medicine, VA Medical Center, St. Louis, MO, USA; Department of Cell Biology and Physiology, Washington University School of Medicine, St. Louis, MO, USA. Electronic address:
Targeting optimal glycemic control based on hemoglobin A1c (A1c) values reduces but does not abolish the onset of diabetic kidney disease and its progression to chronic kidney disease (CKD). This suggests that factors other than the average glucose contribute to the residual risk. Vitamin D deficiency and frequent episodes of acute hyperglycemia (AH) are associated with the onset of albuminuria and CKD progression in diabetes.
View Article and Find Full Text PDFBiomed Pharmacother
January 2025
Maj Institute of Pharmacology, Polish Academy of Sciences, Department of Neurochemistry, 12 Smetna Str., Krakow 31-343, Poland. Electronic address:
Neuropathic pain is a disorder affecting the somatosensory nervous system. However, this condition is also characterized by significant neuroinflammation, primarily involving CNS-resident non-neuronal cells. A promising target for developing new analgesics is histamine H receptor (HR); thus, we aimed to determine the influence of a novel HR antagonist/inverse agonist, E-98 (1-(7-(4-chlorophenoxy)heptyl)-3-methylpiperidine), on pain symptoms and glia activation in model of neuropathic pain in male mice (chronic constriction injury to the sciatic nerve).
View Article and Find Full Text PDFGac Sanit
January 2025
Health Services Research and Pharmacoepidemiology Unit, Foundation for the Promotion of Health and Biomedical Research of Valencia Region (FISABIO), Valencia, Spain; Spanish Network for Research on Chronicity, Primary Care, and Health Promotion (RICAPPS), Valencia, Spain.
Objective: To evaluate the risk of acute pancreatitis and biliary disease in patients treated with glucagon-like peptide-1 receptor agonists (GLP-1 RA).
Method: Population-based, propensity-weighted, new user, active comparator design study including patients with diabetes and obesity initiating treatment with GLP-1 RA or the comparator group sodium-glucose cotransporter 2 inhibitors (SGLT-2i) in the region of Valencia from 2015 to 2021.
Results: In adjusted, per protocol main analysis, no risk differences were found for acute pancreatitis (HR: 0.
Eur J Med Chem
January 2025
Laboratory of Chemical Biology, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, Jilin, 130022, China; School of Applied Chemistry and Engineering, University of Science and Technology of China, Hefei, Anhui, 230026, China. Electronic address:
Substance use disorders (SUDs) present a critical global health challenge, as current treatment options often prove insufficient, particularly for substances like ketamine and methamphetamine. In this study, we developed a novel immunotherapeutic strategy utilizing protein-free, polymer-based vaccines, with hyperbranched polyethylenimine (Hb-PEI) as a carrier to enhance immune specificity and remove the production of non-specific antibodies. Haptens for ketamine and methamphetamine were covalently conjugated to the Hb-PEI carrier, along with the Toll-like receptor (TLR) 7/8 agonist 1V209, to stimulate targeted humoral immune responses.
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